Desoxypeganine and/or its pharmaceutically acceptable acid addition salts can be used for the treatment of drug dependence. These substances are administered in a controlled manner, preferably in a continuous manner. The pharmaceutical administration form makes controlled release possible for, for example, oral, transdermal or alternatively parenteral administration.
The invention relates to the use of desoxypeganine and its pharmaceutically suitable acid addition salts for the treatment of drug dependence and/or drug addiction. These compounds are released, for example, continuously or otherwise in a controlled manner from appropriate pharmaceutical formulations, which are administered, for example, orally, transdermally or otherwise parenterally. Such administration forms can also make subcutaneous, sublingual or intramuscular administration possible. Finally, administration as an implant is also possible. The term parenteral, however, also comprises other administration forms apart from the oral form, i.e., for example, also rectal, intravenous, intramuscular, intraoperitoneal and nasal administration.
Desoxypeganine or a pharmaceutically acceptable acid addition salt or a mixture of base and salt is used for the substitution therapy of drug addicts such as, for example, opiate addicts, for example heroin addicts or cocaine addicts.
Desoxypeganine has in fact been investigated in detail in the former Soviet Union and its pharmacological actions have been intensively researched; the use according to the invention of a desoxypeganine-containing formulation for the treatment of drug addiction and/or drug dependence, however, has not been described until now. 
Desoxypeganine (1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline) is an alkaloid of the empirical formula C11H12N2 having the above structure, which is contained in plaints from the family Zygophyllaceae. It is commercially obtainable as an acid addition salt (hydrochloride).
On account of its pharmacological properties, desoxypeganine belongs to the group of reversibly acting cholinesterase inhibitor, is closely related in its actions to physostigmine and neostigmine, but is distinguished by particular specific properties. Desoxypeganine in fact inhibits not only acetylcholinesterase, but also monoamine oxidase. This advantage offsets its somewhat lower cholinesterase inhibitory action based on the unit of weight (in comparison with physostigmine).
In contrast to neostigmine, desoxypeganine crosses the blood-brain barrier and antagonizes the cerebral actions of cholonergic toxins. Desoxypeganine is obtained by isolation from the harmel peganum (Peganum harmala) or by synthesis.
Pharmaceutical forms which release the active compounds in a controlled manner are already known in the prior art. The administration of pharmaceutically active compounds by means of such formulations can be carried out orally, transdermally or otherwise parenterally. In medicaments of this type, the desoxypeganine can be present as such or in the form of pharmaceutically acceptable acid addition salts, e.g. as the hydrohalide, in particular hydrochloride or hydrobromide, or as a salt of another pharmaceutically acceptable acid, e.g. as a citrate, tartrate or acetate. These agents furthermore contain, as a rule, excipients, such as vehicles, flow-improving agents, solvents and oils, whose nature and amount varies depending on the presentation form. In general, the content of active compound in the medicament, calculated as free desoxypeganine, is between 0.1 and 50% by weight, preferably 2 and 15% by weight.
The active compound or the active compound mixture is released by the corresponding pharmaceutical formulation over a relatively long period, e.g. for approximately 12, 16, 24, or 72 hours. In special administration forms, the period of active compound release can also extend over more than 3 days.
In principle, transdermal administration of desoxypeganine and its pharmaceutically acceptable acid addition salts is to be preferred to oral or parenteral administration. It is clear that a transdermal therapeutic system (TTS) offers greatly increased safety with respect to improper administration. Thus extraction of the -active compound from the TTS matrix without expert knowledge is not possible. Thus improper parenteral administration by an addict to satisfy his/her addiction represents a significantly lower risk than would be presented, for example, in the case of a solution to be administered orally. Therapy with the aid of a transdernial therapeutic system can be carried out without direct supervision or without the physician. A further advantage is the direct control of the dose delivered by means of the release area. In the case of withdrawal therapy, the necessary doses can be tailored simply to the respective needs of the addict. In addition, the known advantages of transdermal administration are provided, namely:
avoidance of the high pharmaceutical dose necessary in the case of oral administration, which has to take account of the first-pass effect, and
more controllable blood levels.
The object on which the invention is based has now been achieved by a transdermal therapeutic systems (TTS) for the administration of desoxypeganine and/or one of its pharmaceutically acceptable acid addition salts as an active compound for the treatment of drug dependence or drug addiction, having
a self-adhesive stratiforin matrix containing active compound(s), where in or on one side of the matrix
a covering film (backing liner) and in or on the other side of the matrix
a removable film (release liner) are provided.